• Pursuant to our in vitro data that neutrophilic elastase act

  2019-12-02

  

  Pursuant to our in vitro data that neutrophilic elastase activated the elastase-dependent oncolytic virus, we initially hypothesized that tumor-infiltrating neutrophils could be the source for elastase in tumor tissue. However, we did not detect neutrophils in the PANC-1 tumor tissue where we observ

• The enantiomeric ratio ER of chiral

  2019-12-02

  

  The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o

• Granzyme B Inhibitor Z-AAD-CH2Cl mg In the absence of ligand

  2019-12-02

  

  In the absence of ligand RNA, 2CARD of RIG-I is masked by the intramolecular interaction with the helicase domain, showing auto-repressed state [33], [34]. But upon viral RNA binding, 2CARD of RIG-I is exposed to interact with the CARD domain of MAVS (also known as Cardif, IPS-1 or VISA) on mitochon

• br Acknowledgments This work was

  2019-12-02

  

  Acknowledgments This work was supported by Grants from the National Research Foundation (2010-0000782) and the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquityl

• Compounds were screened for their activity against

  2019-11-30

  

  Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo

• br Introduction br Conclusion br Acknowledgments and Funding

  2019-11-30

  

  Introduction Conclusion Acknowledgments and Funding Introduction Reversible protein phosphorylation is an important post-translational modification of proteins regulating many processes in the cell. Approximately one third of the cellular proteome is phosphorylated, and several sites are

• Another milestone in the field is the de

  2019-11-30

  

  Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of C-type natriuretic peptide (1-22) (human, rat, swine) , it has been widely applied as a useful chemical probe to discrim

• br Introduction Hydrogen sulfide H S and nitric oxide

  2019-11-30

  

  Introduction Hydrogen sulfide (H2S) and nitric oxide (NO) are important gasotransmitters in the cardiovascular system and instrumental to the fine control of vascular tone [1] and cellular function [2]. NO is synthesized from l-arginine by calmodulin-dependent endothelial nitric oxide synthase (e

• A comparative analysis of the cleavage

  2019-11-30

  

  A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25

• Even more unambiguous was the relative contribution of

  2019-11-30

  

  Even more unambiguous was the relative contribution of Gq/11 signaling in AngII-mediated transactivation as measured by the ERK1/2 and the BRET-based readout. Although Gq/11 was absolutely required for ERK1/2 phosphorylation following AngII-stimulation, in contrast, we observed a sustained EGFR-Grb2

• The attachment of ubiquitin to RTKs such

  2019-11-30

  

  The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an

• Over the past decade targeting DNA repair

  2019-11-30

  

  Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c

• br Acknowledgements This work was supported by a

  2019-11-30

  

  Acknowledgements This work was supported by a Grant for the Program for the Strategic Research Foundation at Private Universities S1101017 organized by the Ministry of Education, Culture, Sports, Science, and Technology (MEXT), Japan and JSPS KAKENHI Grant Numbers JP22560209 and JP5K05842. The

• Currently phosphodiesterase type PDE inhibitors are used wid

  2019-11-29

  

  Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is

• Our data demonstrate that MPO increased

  2019-11-29

  

  Our data demonstrate that MPO increased ETRB mRNA expression, which translated into an increase in ETRB protein expression, which proved to be dependent on the enzyme\'s catalytic activity. Of importance, addition of MPO was sufficient to increase ETRB expression, revealing that endogenous (endothel

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